Beraprost Patch Using Water-Soluble Polymer Base
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Solution Overview
Problem
Beraprost patches with oily bases have high affinity issues leading to suboptimal transdermal absorption, and adding absorption enhancers worsens formulation properties.
Innovation Solution
A patch comprising beraprost or its salt, a water-soluble polymer, a polyhydric alcohol, and a cross-linking agent, specifically with beraprost sodium, polyacrylic acid, propylene glycol, and aluminum glycinate, to enhance transdermal absorption and formulation properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If an oily base is used in the patch, then the formulation properties are improved, but the transdermal absorption of beraprost deteriorates due to high affinity between the drug and the oily base
Solution Approach 1:
The invention changes the fundamental parameter of the base composition from oily to aqueous. By using water-soluble polymers instead of oil-based adhesives, the patent eliminates the high affinity interaction between beraprost and the base that prevented transdermal absorption, while still maintaining good formulation properties through the aqueous polymer matrix.
Solution Approach 2:
The invention creates a composite aqueous system combining water-soluble polymers (such as polyacrylic acid, carboxyvinyl polymer) with beraprost sodium. This composite material approach allows the formulation to achieve both good physical properties (adhesion, cohesion) and high drug delivery performance by leveraging the specific properties of water-soluble polymers that are incompatible with oily bases.
2Productivity
If an absorption enhancer is added to the oily patch, then the transdermal absorption of beraprost is improved, but the formulation properties deteriorate
Solution Approach 1:
The invention extracts and eliminates the need for absorption enhancers by fundamentally changing the base composition from oily to aqueous. The water-soluble polymer base inherently provides the necessary properties for drug release and skin penetration without requiring additional absorption-enhancing additives, thus avoiding formulation degradation.
3Quantity of substance
If beraprost is administered orally, then the drug availability is ensured, but the blood level rapidly elevates causing side effects
Solution Approach 1:
The invention introduces the patch formulation as an intermediary delivery system between oral administration and direct blood delivery. The transdermal patch acts as a mediator that provides controlled, sustained release of beraprost through the skin, avoiding the rapid blood level elevation associated with oral administration while ensuring adequate drug availability at the target site.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The patch achieves high skin permeability and excellent formulation properties, reducing side effects by maintaining stable drug levels and minimizing skin irritation.
Implementation Method 1
a patch which achieves significantly elevated transdermal absorption of beraprost and has excellent formulation properties can be obtained when beraprost or a pharmacologically acceptable salt thereof is added to an adhesive base comprising a water-soluble polymer, a polyhydric alcohol, and a cross-linking agent
Implementation Method 2
an adhesive base comprising a water-soluble polymer, a polyhydric alcohol, and a cross-linking agent
Data Source
AI summary
The present invention provides a patch containing beraprost or a pharmacologically acceptable salt thereof, which achieves high transdermal absorption of beraprost or a pharmacologically acceptable salt thereof and has excellent formulation properties.